Abstract
A series of PF-8380 analogs, a recently developed autotaxin inhibitor, was explored. Inhibition of autotaxin by these analogs, as well as by all PF-8380 synthetic intermediates, shows the importance of meta-dichlorobenzyl and benzo[d]oxazol-2(3H)-one fragments. However, analogs 8 and 9, bearing only the benzo[d]oxazol-2(3H)-one moiety, are more cytotoxic on the LN229 glioblastoma cell line than PF-8380 and temozolomide (TMZ).
Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents* / chemical synthesis
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Antineoplastic Agents* / chemistry
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Antineoplastic Agents* / pharmacology
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Benzoxazoles* / chemical synthesis
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Benzoxazoles* / chemistry
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Benzoxazoles* / pharmacology
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Brain Neoplasms / enzymology
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Brain Neoplasms / pathology
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Cell Line, Tumor
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Cell Survival / drug effects
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Drug Design
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Glioblastoma / enzymology
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Glioblastoma / pathology
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Humans
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Molecular Structure
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Phosphodiesterase Inhibitors* / chemical synthesis
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Phosphodiesterase Inhibitors* / chemistry
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Phosphodiesterase Inhibitors* / pharmacology
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Phosphoric Diester Hydrolases / metabolism*
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Piperazines* / chemical synthesis
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Piperazines* / chemistry
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Piperazines* / pharmacology
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Structure-Activity Relationship
Substances
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6-(3-(piperazin-1-yl)propanoyl)benzo(d)oxazol-2(3H)-one
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Antineoplastic Agents
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Benzoxazoles
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Phosphodiesterase Inhibitors
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Piperazines
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Phosphoric Diester Hydrolases
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alkylglycerophosphoethanolamine phosphodiesterase